Although a great progress has been achieved in the science of oncology, so far, cancer is still the most serious problem in the world threaten public health. It is predicted that new cancer cases will increase to more than 20 million in 2030 in the worldwide from 12.7 million in 2008. Tumor has become the first killer of human health. “Poor cancer” maintains a high incidence, and “rich cancer” also increases rapidly. Cancer spectrum in China is transitioning from the high-incidence in developing countries to the high-incidence in developed countries. The factors responsible for the tendency toward the young among cancer patient in China include environmental pollution, unhealthy life style, high mental stress and the like. Meanwhile, another factor for the serious situation of cancer is rapid aging of population.
Currently, the clinical means for treating cancer include surgery, radiotherapy and chemotherapy. Although these means are therapeutically effective to some extent, they bring about enormous physical and mental sufferings to patients due to great toxic and side-effects. In addition, another important problem that affects the chemotherapeutic effect is the tolerance to cytotoxic agents. Some cancer cells not only tolerated one anti-tumor agent, but also resist to agents of a totally different class, which is the main factor for the failure of the treatment of tumor with chemical agents (chemotherapy). For many anti-tumor agents of natural source, such as alkaloids (colchicine, vinblastine, harringtonine, taxol, etc.), anthracycline antibiotics (adriamycin and daunorubicin), epipodophyllotoxins (Vp-16 and VM-26), and synthetic agents (mitoxantrone and amsacrine), MDR is apt to occur. Even for newly discovered agents, such as paclitaxel and STI-571 for treating chronic myeloid leukemia, drug-resistant are found soon after being applied in clinic, which makes the problem more serious.
However, there is a great difference in signaling pathway between normal cells and tumor cells, which provides a new opportunity for development of anti-tumor agents having the characteristics such as tumor-targeting, high efficiency, and low toxicity. Up to now, there is still no report concerning the derivatives of 15-oxospiramilactone (S-3) of the invention in the prior art.